KR930000468A - 시클로프로펜온 유도체 - Google Patents

시클로프로펜온 유도체 Download PDF

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KR930000468A
KR930000468A KR1019920011134A KR920011134A KR930000468A KR 930000468 A KR930000468 A KR 930000468A KR 1019920011134 A KR1019920011134 A KR 1019920011134A KR 920011134 A KR920011134 A KR 920011134A KR 930000468 A KR930000468 A KR 930000468A
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group
optionally substituted
pharmaceutical composition
compound
hydrogen atom
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KR1019920011134A
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KR100254930B1 (ko
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료오이찌 안도오
야스히로 모리나까
지즈꼬 다까하시
요시구니 다마오
아끼히로 도베
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에도오 다께도시
미쓰비시 가세이 가부시기가이샤
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    • C07C235/72—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms
    • C07C235/76—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton
    • C07C235/78—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of an unsaturated carbon skeleton the carbon skeleton containing rings
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    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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Abstract

내용 없음

Description

시클로프로펜온 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (33)

  1. 아래의 일반 구조식(Ⅰ)의 시클로프로펜온 유도체 또는 약제학적으로 허용되는 그 염.
    위의 식에서, R1은 수소 원자, R12-CO-, R12-O-CO-, R12-NH-CO- 또는 R12-SO2- (여기서 R12는, C3-C15시클로알킬 그룹, 임의로 치환된 C6-C14아릴 그룹, 임의로 치환된 C3-C15시클로알킬옥시 그룹, 임의로 치환된 C6-C14아릴옥시 그룹, 임의로 치환된 C6-C14아릴티오 그룹, 임의로 치환된 C6-C14아릴술포닐 그룹, 임의로 치환된 C7-C20아랄킬옥시 그룹, 임의로 치환된 헤테로환 그룹, 옥소 그룹, 히드록실 그룹, C1-C10알콕시카르보닐 그룹 및 카르복실 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C20알킬 그룹; 임의로 치환된 C3-C15시클로알킬 그룹; 임의로 치환된 C6-C14아릴 그룹 또는 임의로 치환된 헤테로환 그룹이다)이고; R2, R4및 R6은 각각 독립하여 수소 원자이거나 C1-C5알콕시 그룹 또는 C1-C5알킬티오 그룹으로 임의로 치환된 C1-C10알킬 그룹이며; R3, R5및 R7은 각각 독립하여 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C20알킬 그룹, C3-C10시클로알킬 그룹 또는 임의로 치환된 C7-C20아랄킬 그룹이고; R8은 수소 원자 또는 C1-C20알킬 그룹이며; R7과 R8은 함께 C3-C15시클로알킬 그룹을 형성하여도 좋고; R9는 히드록실 그룹 또는 C2-C10아실옥시 그룹이며; R10은 수소 원자이고; 또는 R9와 R10은 함께 옥소 그룹을 형성하여도 좋고; R11은 수소 원자, C3-C15시클로알킬 그룹으로 임의로 치환된 C1-C20알킬 그룹, C3-C15시클로알킬 그룹, C2-C20알케닐 그룹, 임의로 치환된 C6-C14아릴 그룹, 임의로 치환된 C7-C20아랄킬 그룹, 임의로 치환된 헤테로환 그룹 또는 -C(R13)(R14)-OH (여기서 R13및 R14는 각각 독립하여 수소 원자, C1-C20알킬 그룹, 임의로 치환된 C7-C20아랄킬 그룹 또는 임의로 치환된 C6-C14아릴 그룹이거나, R13과 R14는 함께 C3-C15시클로알킬 그룹을 형성하여도 좋다)이며; n은 0 또는 1이다.
  2. 제1항에 있어서, R1은 수소 원자, R12-CO-, R12-O-CO-, R12-NH-CO- 또는 R12-SO2- (여기서 R12는, C3-C15시클로알킬 그룹, 임의로 치환된 C6-C14아릴 그룹, 임의로 치환된 C6-C14아릴옥시 그룹, 임의로 치환된 C6-C14아릴티오 그룹, 임의로 치환된 C7-C20아랄킬옥시 그룹, 임의로 치환된 헤테로환 그룹, 옥소 그룹, 히드록실 그룹, C1-C10알콕시카르보닐 그룹 및 카르복실 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C20알킬 그룹, C3-C15시클로알킬 그룹, 임의로 치환된 C6-C14아릴 그룹 또는 임의로 치환된 헤테로환 그룹이다)이고; R2, R4및 R6은 각각 독립하여 수소 원자 또는 C1-C5알킬티오 그룹으로 임의로 치환된 C1-C10알킬 그룹이며; R3, R5및 R7은 각각 독립하여 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C20알킬 그룹, C3-C10시클로알킬 그룹 또는 임의로 치환된 C7-C20아랄킬 그룹이고; R8은 수소 원자 또는 C1-C20알킬 그룹이며; R11은 수소 원자, C3-C15시클로알킬 그룹으로 임의로 치환된 C1-C20알킬 그룹, C3-C15시클로알킬 그룹, C2-C20알케닐 그룹, 임의로 치환된 C6-C14아릴 그룹, C7-C20아랄킬 그룹, 임의로 치환된 헤테로환 그룹 또는 -C(R13)(R14)-OH (여기서 R13과 R14는 각각 독립하여 수소 원자, C1-C20알킬 그룹 또는 C6-C14아릴 그룹)인 화합물.
  3. 제2항에 있어서, R1은 R12-CO-, R12-O-CO-, R12-NH-CO- 또는 R12-SO2- (여기서 R12는, C3-C10시클로알킬 그룹, 임의로 치환된 C6-C14아릴 그룹, 임의로 치환된 C6-C14아릴옥시 그룹, 임의로 치환된 C6-C14아릴티오 그룹, 임의로 치환된 C7-C20아랄킬옥시 그룹, 임의로 치환된 헤테로환 그룹 및 옥소 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C15알킬 그룹, C3-C10시클로알킬 그룹, C6-C14아릴 그룹 또는 임의로 치환된 헤테로환 그룹이다)이고; R2, R4및 R6은 각각 독립하여 수소 원자 또는 C1-C10알킬 그룹이며; R3, R5및 R7은 각각 독립하여 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C15알킬 그룹, C3-C10시클로알킬 그룹 또는 임의로 치환된 C7-C20아랄킬 그룹이고; R8은 수소 원자이고; R9는 히드록실 그룹 또는 C2-C10아실옥시 그룹이며; R10은 수소 원자이고; R11은 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C15알킬 그룹, C3-C10시클로알킬 그룹, C7-C20아랄킬 그룹, 임의로 치환된 C6-C10아릴 그룹 또는 임의로 치환된 헤테로환 그룹인 화합물.
  4. 제3항에 있어서, R1은 R12-CO-, R12-O-CO-, R12-NH-CO- (여기서 R12는, C3-C10시클로알킬 그룹, 임의로 치환된 C6-C14아릴 그룹, 임의로 치환된 C6-C14아릴옥시 그룹, 임의로 치환된 C6-C14아릴티오 그룹, 임의로 치환된 C7-C20아랄킬옥시 그룹, 임의로 치환된 헤테로환 그룹 및 옥소 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C15알킬 그룹이거나 임의로 치환된 C6-C10아릴 그룹이다)이고; R3, R5및 R7은 각각 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C15알킬 그룹, C3-C10시클로알킬 그룹 또는 C7-C20아랄킬 그룹인 화합물.
  5. 제4항에 있어서, R1은 R12-O-CO- (여기서 R12는, C3-C10시클로알킬 그룹, C6-C14아릴 그룹 및 헤테로환 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C15알킬 그룹이거나 C3-C10시클로알킬 그룹이다)이고; R4와 R6은 각각 수소 원자이며; R11은 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C15알킬 그룹, C3-C10시클로알킬 그룹 또는 C7-C20아랄킬 그룹, C6-C10아릴 그룹이고; n은 0인 화합물.
  6. 제4항에 있어서, R1은 R12-CO- (여기서 R12는, C3-C10시클로알킬 그룹, C6-C14아릴 그룹 및 헤테로환 그룹으로 된 군으로부터 선택되는 치환기 하나 이상으로 임의로 치환된 C1-C15알킬 그룹이다)이고; R4와 R6은 각각 수소 원자이며; R5와 R7은 각각 독립하여 수소 원자, C3-C10시클로알킬 그룹으로 임의로 치환된 C1-C15알킬 그룹 또는 C7-C20아랄킬 그룹이고, R9는 히드록실 그룹이고; R11은 임의로 치환된 헤테로환 그룹이고; n은 0인 화합물.
  7. 제3항에 있어서, R1은 R12-SO2-이고, R11은 수소 원자, 임의로 치환된 C6∼C10아릴 그룹 또는 임의로 치환된 헤테로환 그룹인 화합물.
  8. 제7항에 있어서, R12는 임의로 치환된 C6∼C10아릴 그룹 또는 임의로 치환된 헤테로환 그룹인 화합물.
  9. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.
  10. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 티올 프로테아제의 이상 긴장에 의한 질환 치료용의 약제학적 조성물.
  11. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 골격근 허탈로 인한 질환치료용 약제학적 조성물.
  12. 제11항에 있어서, 골격근의 허탈로 인한 질환이 근이영양증인 약제학적 조성물.
  13. 제11항에 있어서, 골격근의 허탈로 인한 질환이 근위축증인 약제학적 조성물.
  14. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 국소 빈혈병 질환 치료용의 약제학적 조성물.
  15. 제14항에 있어서, 국소 빈혈증 질환이 심장 경색인 약제학적 조성물.
  16. 제14항에 있어서, 국소 빈혈증 질환이 졸증인 약제학적 조성물.
  17. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 뇌손상에 의한 의식장해 또는 운동장해 치료용의 약제학적 조성물.
  18. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 신경세포의 수초 탈락에 의한 질환 치료용의 약제학적 조성물.
  19. 제18항에 있어서, 신경세포의 수초 탈락에 의한 질환이 다발성 경화증인 약제학적 조성물.
  20. 제18항에 있어서, 신경세포의 수초 탈락에 의한 질환이 말초 신경의 신경병인 약제학적 조성물.
  21. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 백내장 치료용의 약제학적 조성물.
  22. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 염증 치료용의 약제학적 조성물.
  23. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 알레르기 질환 치료용의 약제학적 조성물.
  24. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 간장 질환 치료용의 약제학적 조성물.
  25. 제24항에 있어서, 간장 질환이 전격성 간염인 약제학적 조성물.
  26. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 골다공증 치료용의 약제학적 조성물.
  27. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 과칼슘혈증 치료용의 약제학적 조성물.
  28. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 성호르몬 수용체의 비정상적 활성화에 기인한 질환 치료용의 약제학적 조성물.
  29. 제28항에 있어서, 성호르몬 수용체의 비정상적 활성화에 기인한 질환이 유방암인 약제학적 조성물.
  30. 제28항에 있어서, 성호르몬 수용체의 비정상적 활성화에 기인한 질환이 전립선암인 약제학적 조성물.
  31. 제28항에 있어서, 성호르몬 수용체의 비정상적 활성화에 기인한 질환이 전립선 비대증인 약제학적 조성물.
  32. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 종양 전이 예방 또는 종양 세포 성장 억제용의 약제학적 조성물.
  33. 활성 성분으로서의 제1항의 화합물과 약제학적으로 허용되는 담체를 함유하는 혈소판 응집 억제용의 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019920011134A 1991-06-25 1992-06-25 시클로프로펜온 유도체 KR100254930B1 (ko)

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